Literature DB >> 22056746

Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.

Thomas M Kirrane1, Stephen J Boyer, Jennifer Burke, Xin Guo, Roger J Snow, Lida Soleymanzadeh, Alan Swinamer, Yunlong Zhang, Jeffery B Madwed, Mohammed Kashem, Stanley Kugler, Margaret M O'Neill.   

Abstract

A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This led to the identification of compound 24, BIX 02565, an attractive candidate for use in vitro and in vivo to explore the role of RSK as a target for the treatment heart failure.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 22056746     DOI: 10.1016/j.bmcl.2011.10.029

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  The RSK Inhibitor BIX02565 Limits Cardiac Ischemia/Reperfusion Injury.

Authors:  Xi Shi; Margaret M O'Neill; Scott MacDonnell; Paul S Brookes; Chen Yan; Bradford C Berk
Journal:  J Cardiovasc Pharmacol Ther       Date:  2015-06-30       Impact factor: 2.457

2.  Development of a RSK Inhibitor as a Novel Therapy for Triple-Negative Breast Cancer.

Authors:  Katarzyna A Ludwik; J Preston Campbell; Mingzong Li; Yu Li; Zachary M Sandusky; Lejla Pasic; Miranda E Sowder; David R Brenin; Jennifer A Pietenpol; George A O'Doherty; Deborah A Lannigan
Journal:  Mol Cancer Ther       Date:  2016-08-15       Impact factor: 6.261

3.  Structural and functional basis for p38-MK2-activated Rsk signaling in toll-like receptor-stimulated dendritic cells.

Authors:  Rossana Zaru; Alexander J Edgar; André Hanauer; Colin Watts
Journal:  Mol Cell Biol       Date:  2014-10-20       Impact factor: 4.272

4.  Bacterial Expression, Purification and In Vitro Phosphorylation of Full-Length Ribosomal S6 Kinase 2 (RSK2).

Authors:  Darkhan Utepbergenov; Paulina M Hennig; Urszula Derewenda; Mykhaylo V Artamonov; Avril V Somlyo; Zygmunt S Derewenda
Journal:  PLoS One       Date:  2016-10-12       Impact factor: 3.240

5.  Targeting oncoproteins with a positive selection assay for protein degraders.

Authors:  Vidyasagar Koduri; Leslie Duplaquet; Benjamin L Lampson; Adam C Wang; Amin H Sabet; Mette Ishoey; Joshiawa Paulk; Mingxing Teng; Isaac S Harris; Jennifer E Endress; Xiaoxi Liu; Ethan Dasilva; Joao A Paulo; Kimberly J Briggs; John G Doench; Christopher J Ott; Tinghu Zhang; Katherine A Donovan; Eric S Fischer; Steven P Gygi; Nathanael S Gray; James Bradner; Jeffrey A Medin; Sara J Buhrlage; Matthew G Oser; William G Kaelin
Journal:  Sci Adv       Date:  2021-02-05       Impact factor: 14.957

6.  A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870.

Authors:  Alexander J Edgar; Matthias Trost; Colin Watts; Rossana Zaru
Journal:  Biosci Rep       Date:  2014-02-01       Impact factor: 3.840

Review 7.  RSK Isoforms in Acute Myeloid Leukemia.

Authors:  Minyoung Youn; Jesus Omar Gomez; Kailen Mark; Kathleen M Sakamoto
Journal:  Biomedicines       Date:  2021-06-24
  7 in total

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